Antiviral nucleosides
    2.
    发明授权
    Antiviral nucleosides 有权
    抗病毒核苷

    公开(公告)号:US07825239B2

    公开(公告)日:2010-11-02

    申请号:US12690842

    申请日:2010-01-20

    Abstract: 4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.

    Abstract translation: 4-氨基-1 - ((2R,3S,4S,5R)-5-叠氮基-4-羟基-5-羟甲基-3-甲基 - 四氢 - 呋喃-2-基)-1H-嘧啶-2-酮( 22)及其前药是丙型肝炎(HCV)聚合酶抑制剂。 还公开了用于抑制HCV和治疗HCV介导的疾病的组合物和方法,用于制备该方法中使用的化合物和合成中间体的方法。

    ANTIVIRAL NUCLEOSIDES
    5.
    发明申请
    ANTIVIRAL NUCLEOSIDES 有权
    抗性核苷酸

    公开(公告)号:US20100130735A1

    公开(公告)日:2010-05-27

    申请号:US12690842

    申请日:2010-01-20

    Abstract: 4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.

    Abstract translation: 4-氨基-1 - ((2R,3S,4S,5R)-5-叠氮基-4-羟基-5-羟甲基-3-甲基 - 四氢 - 呋喃-2-基)-1H-嘧啶-2-酮( 22)及其前药是丙型肝炎(HCV)聚合酶抑制剂。 还公开了用于抑制HCV和治疗HCV介导的疾病的组合物和方法,用于制备该方法中使用的化合物和合成中间体的方法。

    Phosphoramidate derivatives of nucleosides
    8.
    发明授权
    Phosphoramidate derivatives of nucleosides 有权
    核苷的氨基磷酸衍生物

    公开(公告)号:US08552021B2

    公开(公告)日:2013-10-08

    申请号:US13498459

    申请日:2010-09-29

    CPC classification number: C07H19/10

    Abstract: Compounds of formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen, —C(═O)R6 or —C(═O)CHR7—NH2; R2 is hydrogen; or C1-C6alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C1-C6alkyl, C2-C6-alkenyl and C1-C6alkoxy, hydroxy or amino, or R2 is naphtyl; or R2 is indolyl, R3 is hydrogen, C1-C6alkyl, benzyl; R4 is hydrogen, C1-C6alkyl, benzyl; or R3 and R4 together with the carbon atom to which they are attached form C3-C7cycloalkyl; R5 is C1-C10alkyl, C3-C7-cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C1-C6alkoxy, amino, mono- and diC1-C6alkylamino; R6 is C1-C6 alkyl; R7 is C1-C6 alkyl; R8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.

    Abstract translation: 式I化合物:包括其任何可能的立体异构体,其中:R 1是氢,-C(= O)R 6或-C(= O)CHR 7 -NH 2; R2是氢; 或任选被1,2或3个独立地选自卤素,C 1 -C 6烷基,C 2 -C 6 - 烯基和C 1 -C 6烷氧基,羟基或氨基的取代基取代的C 1 -C 6烷基或苯基,或者R 2是萘基; 或R 2为吲哚基,R 3为氢,C 1 -C 6烷基,苄基; R4是氢,C1-C6烷基,苄基; 或R 3和R 4与它们所连接的碳原子一起形成C 3 -C 7环烷基; R5是C1-C10烷基,C3-C7-环烷基,苄基或苯基,其中任何一个任选被1,2或3个独立地选自羟基,C 1 -C 6烷氧基,氨基,单和二C 1 -C 6烷基氨基的取代基取代; R6是C1-C6烷基; R7是C1-C6烷基; R8是氢或卤素; 或其药学上可接受的盐或溶剂化物可用于预防或治疗HCV感染。

    Phosphoramidate Derivatives of Nucleosides
    9.
    发明申请
    Phosphoramidate Derivatives of Nucleosides 有权
    核苷酸的氨基磷酸衍生物

    公开(公告)号:US20120225839A1

    公开(公告)日:2012-09-06

    申请号:US13498459

    申请日:2010-09-29

    CPC classification number: C07H19/10

    Abstract: Compounds of formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen, —C(═O)R6 or —C(═O)CHR7—NH2; R2 is hydrogen; or C1-C6alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C1-C6alkyl, C2-C6-alkenyl and C1-C6alkoxy, hydroxy or amino, or R2 is naphtyl; or R2 is indolyl, R3 is hydrogen, C1-C6alkyl, benzyl; R4 is hydrogen, C1-C6alkyl, benzyl; or R3 and R4 together with the carbon atom to which they are attached form C3-C7cycloalkyl; R5 is C1-C10alkyl, C3-C7-cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C1-C6alkoxy, amino, mono- and diC1-C6alkylamino; R6 is C1-C6 alkyl; R7 is C1-C6 alkyl; R8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.

    Abstract translation: 式I化合物:包括其任何可能的立体异构体,其中:R 1是氢,-C(= O)R 6或-C(= O)CHR 7 -NH 2; R2是氢; 或任选被1,2或3个独立地选自卤素,C 1 -C 6烷基,C 2 -C 6 - 烯基和C 1 -C 6烷氧基,羟基或氨基的取代基取代的C 1 -C 6烷基或苯基,或者R 2是萘基; 或R 2为吲哚基,R 3为氢,C 1 -C 6烷基,苄基; R4是氢,C1-C6烷基,苄基; 或R 3和R 4与它们所连接的碳原子一起形成C 3 -C 7环烷基; R5是C1-C10烷基,C3-C7-环烷基,苄基或苯基,其中任何一个任选被1,2或3个独立地选自羟基,C 1 -C 6烷氧基,氨基,单和二C 1 -C 6烷基氨基的取代基取代; R6是C1-C6烷基; R7是C1-C6烷基; R8是氢或卤素; 或其药学上可接受的盐或溶剂化物可用于预防或治疗HCV感染。

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